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395 B 536 Winstal. O. Saito EEEEEE USOO8426439B2 (12) UnitedO States Patent (10) Patent No.: US 8.426,439 B2 Ciccocioppo (45) Date of Patent: *Apr. 23, 2013 (54) COMPOSITIONS AND METHODS FOR 7,510,728 B2 3/2009 Koike ........................... 424/464 PROPHYLAXIS AND TREATMENT OF 7,517,900 B2 4/2009 Pendri et al. ... 514,404 7,524,975 B2 4/2009 Mae et al. ... 549,405 ADDCTIONS 2002fOOO6942 A1 1/2002 Davis ........... ... 514,369 2002fOO77320 A1 6/2002 Lohray et al. 514/226.2 (75) Inventor: Roberto Ciccocioppo, Camerino (IT) 2003/0069246 A1 4/2003 Darrow et al. ................ 514,245 2003/010.0587 A1 5/2003 Moinet et al. ................. 514,369 (73) Assignee: Omeros Corporation, Seattle, WA (US) 2003/0220373 Al 1 1/2003 Jaye et al. ... 514,342 2004/0028735 A1 2/2004 Kositprapa ... 424/468 2004/OO77525 A1 4/2004 Chapman et al. ... 514/2 - r 2004/0096499 A1 5/2004 Vaya et al. ... 424/468 (*) Notice: Subject to any disclaimer, the term of this 2004/0127443 A1 7/2004 Pershadsingh 514,44 patent is extended or adjusted under 35 2004/0204472 A1 10/2004 Briggs et al. 514,406 U.S.C. 154(b) by 859 days. 2005, 00041 79 A1 1/2005 Pedersen ...... ... 514,342 2005, OO14786 A1 1/2005 Sun et al. .. ... 514/313 This patent is Subject to a terminal dis- 2005, OO 14833 A1 1/2005 Clark et al. .. ... 514,561 claimer. 2005, 0096331 A1 5/2005 Das et al. 514,259.3 2005, 01711.1.0 A1 8, 2005 Yu et al. ....... ... 514,248 2006, OOO9518 A1 1/2006 Campbell et al. ... 514,522 (21) Appl. No.: 12/101,943 2006/0024365 A1 2/2006 Vaya et al. ... 424/468 (22) Filed: Apr. 11, 2008 2006/0059152 A1 3/2006 Nakamura ........................ 707/7 (Continued) (65) Prior Publication Data FOREIGN PATENT DOCUMENTS CA 2589 393 12/2007 US 2009/0048232A1 Feb. 19, 2009 EP 1867994 A2 12/2007 (Continued) Related U.S. Application Data OTHER PUBLICATIONS Cohen et al. CB1 receptor antagonists for the treatment of nicotine (60) Provisional application No. 60/911,201, filed on Apr. addiction. Pharmacology, Biochemistry and Behavior 81. 387-395 11, 2007. (2005).* Ang, E. et al., “Induction of nuclear factor-kappaB in nucleus (51) Int. Cl. accumbens by chronic cocaine administration.” J. of Neurochem. A6 IK3I/44 (2006.01) 79:221-224, 2001. (52) U.S. Cl. Asanuma, M. et al., “Methamphetamine-induced increase in USPC S14/293: 514/342: 514/811 striatalNF-kappaB DNA-binding activity is attenuated in Superoxide (58) Field of- -Classification - - - - - - - - - - - - - - - - - - - - - - - Search- - - ..................s s s1420s, dismutaseStase trrangenic ic mice,mice.” Molecular trainBrain researcR h 60:305-309, 514/342,811 Ashby, C. et al., “Acute Administration of the Selective D. Receptor See application file for complete search history. Antagonist SB-27701 1A Blocks the Acquisition and Expression of the Conditioned Place Preference Response to Heroin in Male Rats.” (56) References Cited Synapse 48:154-156, 2003. Continued U.S. PATENT DOCUMENTS ( ) 4,572,912 A 2/1986 Yoshioka et al. ............. so Primary Examiner - Barbara P Badio 4,582,839 A 4, 1986 Meguro et al. 514/342 Assistant Examiner — Sara E Townsley 4,687,777 A 8/1987 Meguro et al. 514,342 (74) Attorney, Agent, or Firm — Marcia S. Kelbon 4,725,610 A 2/1988 Meguro et al. 514,369 4,775,687. A 10/1988 Meguro et al. 514/369 (57) ABSTRACT 4,812,570 A 3/1989 Meguro et al. 546,280 The present invention relates to methods of treating or pre 5,965,584. A 10/1999 Ikeda et al. 514,342 venting addiction and relapse use of addictive agents, and g h '' A 58 With . SS treating or preventing addictive or compulsive behavior and k - W Cai Ca. 6,437,143395 B2B 5368/2002 MoinetWinstal. et al. ..O. ... Saito548, 183 EEEEEEg a p some p ited recept 6,506,762 B1 1/2003 Horvath et al. 514,2594 gamma (PPARy). agonist, alone or in combination with 6,582,738 B2 6/2003 Gubler .............................. 426, 5 another therapeutic agent, such as, for example, an opioid 6,620,830 B2 9/2003 Chiang .............. 514,369 receptor antagonist or an antidepressant. The present inven 6,794,154 B1 9/2004 Yamanouchi et al. 435/7.8 tion also includes pharmaceutical compositions for treating 7,037,910 B2 5/2006 Ewing et al. .................. 514,243 or preventing addiction or relapse that include a PPARYago 7,067,530 B2 6/2006 Jeppesen et al. ........... 514,311 nist and one or more other therapeutic agents, as well as unit 7,141,561 B2 11/2006 Schwinket al.......... 51421203 dosage forms of Such pharmaceutical compositions, which 7.312,229 B2 12/2007 Dankulich et al. ............ 514/284 contain a dosage effective in treating or preventing addiction 7,319, 170 B2 1/2008 Sahoo et al. ....... ... 564/43 1 Th thods and iti fthei ti 7,326,706 B2 2/2008 Ellsworth et al. .. 514,241 orrelapse. I nemeunoas and compositions oIune invention are 7,335,799 B2 2/2008 Dasseux et al. .... ... 568,861 useful in the treatment or prevention of addiction to any agent, 7,365,064 B2 4/2008 Bhuniya et al. 514,230.5 including alcohol, nicotine, marijuana, cocaine, and amphet 7,378.418 B2 5, 2008 Yu et al. ............. ... 514,248 amines, as well as compulsive and addictive behaviors, 7,381,736 B2 6/2008 Cheruvallath et al. ........ 514,370 including pathological gambling and pathological overeat 7,411,071 B2 8/2008 Yang et al. .................... 548,195 ing 7,429,575 B2 9, 2008 Yu et al. ......... 514,114 7,446,110 B2 11/2008 Kaufman et al. ............. 514,284 38 Claims, 25 Drawing Sheets US 8,426.439 B2 Page 2 U.S. PATENT DOCUMENTS WO WO 2007/039 125 4/2007 2006, OO84686 A1 4/2006 Barak ........................... 514,357 W. W. 3:29:25 5392 2006, O148721 A1 7/2006 Erondu. ................. ... 514/23 WO WO 2007/079239 7/2007 2006.0167045 A1 7/2006 Waldstreicher et al. 514,311 WO WO 2007/082206 7/2007 2006/0211749 A1 9, 2006 Bobotas et al. .... 514,369 WO WO 2007/083.146 7/2007 2006/0252670 A1 11/2006 Fiorucci et al. ................... 514/3 WO WO 2007/106862 9, 2007 2006/0270722 A1 1 1/2006 Thornberry et al. 514,374 WO WO 2007 120605 10/2007 2007/0O37882 A1 2/2007 Kita et al. .......... ... 514,548 WO WO 2007.121545 11, 2007 2007.0049576 A1* 3, 2007 Barlow et al. 514,214.03 WO WO 2007/126135 11, 2007 2007/004.9613 A1 3/2007 Chen et al. .. ... 514,290 WO WO 2007.1366O7 11, 2007 2007/0060547 A1 3/2007 Campbell et al. ... 514,64 WO WO 2008/OOO643 1, 2008 2007/0066630 A1 3/2007 Palani et al. ... 514,260.1 WO WO 2008/OO8433 1, 2008 2007.0099884 A1 5, 2007 Erondu et al. ... 514, 183 WO WO 2008/O13384 1, 2008 2007/01 12070 A1 5/2007 Aubert et al. ................. 514,534 WO WO 2008/O17398 2, 2008 2007/0167435 A1 7/2007 Mutahi et al. ................. 514,218 WO WO 2008/024284 2, 2008 2007/0167468 A1 7/2007 Schoenafinger et al. .. 514/263.2 WO WO 2008/024456 2, 2008 2007/O197606 A1 8/2007 Burczynski et al. .......... 514/342 WO WO 2008/030604 A2 3, 2008 2007/0213359 A1 9/2007 Burstein et al. ............... 514,300 WO WO 2008/030618 3, 2008 2007/0232573 A1 10, 2007 Patell et al. ................... 514,125 WO WO 2008/030651 3, 2008 2007/0238757 A1 10/2007 Chapman et al. 514,342 WO WO 2008/O5325.6 A1 5, 2008 2007/0276041 A1 11/2007 Oonuki et al. ... 514,563 WO WO 2008/063.842 5, 2008 2007,0299047 A1 12, 2007 Maher et al. 514,210.02 WO WO 2008/095263 8, 2008 2008, OO19978 A1 1/2008 Palani et al. ... 424,158.1 WO WO 2008/128126 10, 2008 2008, OO45580 A1 2/2008 Madhavan et all 514,378 WO WO 2008, 133884 11, 2008 2008, OO64671 A1 3/2008 Barlow et al. ................. 514,171 2008/0.103165 A1 5/2008 Barlow et al. ................. 514,297 OTHER PUBLICATIONS 2008/O127972 A1 6, 2008 Morton ....... 128,203.15 Barroso, I. et al., “Dominant negative mutations in human 2008, 0220078 A1 9/2008 Morton et al. ................ 424/490 PPARgamma associated with severe insulin resistance, diabetes mel 2010, O184806 A1 7, 2010 Barlow et al. litus and hypertension.” Nature 402:880-883, 1999. FOREIGN PATENT DOCUMENTS i s TMechanisms of Action of PPARs, Annu. Rev. JP 2008-44932 2, 2008 Bordet, R. et al., “PPAR: a new pharmacological target for KR 10-2007-01 12580 11, 2007 neuroprotection in stroke and neurodegenerative diseases. Bio W. W. 93. 1399. chemical Society 34(Pt6): 1341-1346, 2006. WO WO99.63983 12/1999 Bowers, M. et al., "Forebrain astroglial plasticity is induced follow ing withdrawal from repeated cocaine administration.” European W W 8.25 38: Journal of Neuroscience 17. 1273-1278, 2003. WO WO O2/49626 6, 2002 Breidert, T. et al., “Protective action of the peroxisome proliferator WO WO 03/026586 4/2003 activated receptor-gamma agonist pioglitaZone in a mouse model of WO WO 03/045918 6, 2003 Parkinson's disease.” Journal of Neurochemistry 82.615-624, 2002. WO WO 2004/OOO295 12/2003 Burstein, S., “PPAR-gamma: a nuclear receptor with affinity for WO WO 2004/O10992 2, 2004 cannabinoids.” Life Sciences 77:1674-1684, 2005. WO WO 2004/0781-13 9, 2004 Butcher, S. et al., “Neuroprotetive Actions of FK506 in WO WO 2004/0924.17 10, 2004 Experimentala Stroke: In Vivo evidence against an Antiexcitotoxic W.
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